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Assay Detail

CHEMBL822947

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Steroid potentiation of 5% GABA responses in Xenopus oocytes expressing human alpha-1-beta-2-gamma-2L subunits of GABA-A receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors.
Upasani RB, Yang KC, Acosta-Burruel M, Konkoy CS, McLellan JA, Woodward RM, Lan NC, Carter RB, Hawkinson JE.
J Med Chem (1997) 40 : 73 -84
PubMed 9016330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.60 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3138009 1 8.18
CHEMBL3138433 1 8.09
CHEMBL3138291 1 7.75
CHEMBL3138293 1 7.51
CHEMBL3138017 1 6.47
CHEMBL3138315 1 -
CHEMBL3138292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3138009 EC50 = 6.6 nM 8.18
CHEMBL3138433 EC50 = 8.2 nM 8.09
CHEMBL3138291 EC50 = 18.0 nM 7.75
CHEMBL3138293 EC50 = 31.0 nM 7.51
CHEMBL3138017 EC50 = 340.0 nM 6.47
CHEMBL3138315 EC50 > 1000.0 nM -
CHEMBL3138292 EC50 > 1000.0 nM -